Rosuvastatin: Advanced Lipid Management for Cardiovascular Protection
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Synonyms | |||
Rosuvastatin is a highly potent, synthetic HMG-CoA reductase inhibitor, widely recognized in clinical practice for its efficacy in managing dyslipidemia and reducing cardiovascular risk. As a third-generation statin, it demonstrates superior LDL-cholesterol reduction capabilities compared to earlier agents, making it a cornerstone in both primary and secondary prevention strategies. Its well-characterized pharmacokinetic profile and favorable safety record support its use across diverse patient populations, under appropriate medical supervision.
Features
- Active pharmaceutical ingredient: Rosuvastatin calcium
- Standard dosage strengths: 5 mg, 10 mg, 20 mg, 40 mg tablets
- High hepatic selectivity with minimal cytochrome P450 metabolism (primarily CYP2C9)
- Extended elimination half-life of approximately 19 hours
- Bioavailability of approximately 20%
- Dual excretion pathway (feces 90%, urine 10%)
Benefits
- Achieves rapid and substantial reductions in LDL-cholesterol levels by 45-63% at maximum doses
- Significantly lowers triglyceride levels while raising HDL-cholesterol
- Demonstrates proven reduction in major adverse cardiovascular events
- Exhibits anti-inflammatory effects through CRP reduction
- Shows consistent efficacy across various demographic subgroups
- Provides convenient once-daily dosing regimen supporting medication adherence
Common use
Rosuvastatin is primarily indicated for the management of dyslipidemias, including primary hypercholesterolemia and mixed dyslipidemia. It is extensively used in both primary prevention for patients with multiple risk factors but without established cardiovascular disease, and secondary prevention in patients with documented coronary artery disease, cerebrovascular disease, or peripheral arterial disease. Additionally, it is employed in familial hypercholesterolemia management and as part of comprehensive cardiovascular risk reduction strategies in diabetic patients.
Dosage and direction
The recommended starting dose is typically 10-20 mg once daily, with dosage adjustment based on lipid response and tolerability. For patients requiring aggressive LDL reduction, the maximum approved dose is 40 mg daily. Administration should occur at any time of day, with or without food, though consistency in timing is recommended. Dosage requires adjustment in patients with renal impairment (CrCl <30 mL/min): initial dose should not exceed 5 mg daily. Asian patients may demonstrate increased systemic exposure, warranting consideration of 5 mg as starting dose. Regular lipid monitoring should guide dosage titration, typically performed at 4-week intervals.
Precautions
Liver function tests must be performed before initiation and periodically during therapy. Patients should report unexplained muscle pain, tenderness, or weakness promptly. Caution is advised in patients consuming substantial quantities of alcohol or with history of liver disease. Blood glucose levels should be monitored as statins may increase HbA1c and fasting serum glucose levels. Use with caution in patients with risk factors for myopathy/rhabdomyolysis, including advanced age, renal impairment, and uncontrolled hypothyroidism. Consider temporary discontinuation in patients experiencing major surgery, trauma, or severe metabolic disorders.
Contraindications
Absolute contraindications include active liver disease or unexplained persistent elevations of serum transaminases; pregnancy and breastfeeding; concomitant use with cyclosporine; and hypersensitivity to rosuvastatin or any product components. Relative contraindications include history of statin-induced myopathy, concurrent use of gemfibrozil, and severe renal impairment (CrCl <30 mL/min) not on dialysis.
Possible side effect
Common adverse reactions (≥2%) include headache, myalgia, constipation, nausea, and abdominal pain. Less frequent but clinically significant effects may include: elevated liver enzymes (≥3× ULN in 0.2-0.4% of patients), myopathy (0.2-0.5%), arthralgia, and diabetes mellitus incidence increase. Rare serious adverse events include rhabdomyolysis (<0.1%), immune-mediated necrotizing myopathy, and hemorrhagic stroke. Cognitive effects such as memory impairment and confusion have been reported, though causality remains uncertain.
Drug interaction
Significant interactions occur with cyclosporine (contraindicated), gemfibrozil (avoid combination), and other fibrates (use with caution). Protease inhibitors, particularly combination HIV regimens, may increase rosuvastatin exposure. Warfarin monitoring is recommended due to potential INR elevation. Antacids containing aluminum and magnesium hydroxide decrease rosuvastatin absorption—administer至少 2 hours apart. Moderate interactions possible with erythromycin, oral contraceptives, and niacin.
Missed dose
If a dose is missed, patients should take it as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take double or extra doses to make up for a missed dose. Consistent daily administration is important for maintaining stable lipid control, though occasional missed doses are unlikely to significantly impact long-term efficacy.
Overdose
No specific antidote exists for rosuvastatin overdose. Management should be supportive and symptomatic. In cases of recent ingestion, gastric lavage may be considered along with activated charcoal administration. Liver function and CPK levels should be monitored closely. Hemodialysis is unlikely to be effective due to high protein binding. Cases of overdose have reported symptoms including gastrointestinal distress, elevated transaminases, and myalgia. Medical supervision is recommended for any suspected overdose situation.
Storage
Store at controlled room temperature (20-25°C/68-77°F) with excursions permitted between 15-30°C (59-86°F). Protect from light and moisture. Keep in original container with lid tightly closed. Do not store in bathroom or other humid areas. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Properly discard any unused medication through take-back programs or following FDA-recommended disposal methods.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Rosuvastatin is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to therapy may vary, and appropriate monitoring is essential. Patients should consult their healthcare provider for personalized medical advice, including potential risks and benefits specific to their clinical situation. Never initiate, discontinue, or change dosage without medical supervision.
Reviews
Clinical trials consistently demonstrate rosuvastatin’s efficacy in lipid management, with the JUPITER trial showing 44% reduction in major cardiovascular events in patients with elevated CRP. Meta-analyses confirm its superior LDL-lowering potency compared to other statins. Real-world evidence supports maintained efficacy in diverse populations, though careful attention to dose-related side effects remains important in clinical practice. Long-term extension studies show sustained lipid-lowering effects and generally favorable safety profile over treatment durations exceeding five years.